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Bronchodilators and Other

Respiratory Agents

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Drugs Affecting
the Respiratory System
• Bronchodilators
– Xanthine derivatives
– Beta-agonists

• Anticholinergics
• Antileukotriene agents
• Corticosteroids
• Mast cell stabilizers
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
Instructors may want to use
EIC Image #94:

Airway Restrictive Factors

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Bronchodilators: Xanthine Derivatives

• Plant alkaloids: caffeine, theobromine, and


theophylline
• Only theophylline is used as a bronchodilator
Examples: aminophylline
dyphilline
oxtriphylline
theophylline (Bronkodyl, Slo-bid,
Theo-Dur,Uniphyl)

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Bronchodilators: Xanthine Derivatives
Mechanism of Action

• Increase levels of energy-producing cAMP*


• This is done competitively inhibiting
phosphodiesterase (PDE), the enzyme that
breaks down cAMP
• Result: decreased cAMP levels, smooth
muscle relaxation, bronchodilation, and
increased airflow
*cAMP = cyclic adenosine monophosphate

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Bronchodilators: Xanthine Derivatives
Drug Effects

• Cause bronchodilation by relaxing smooth muscles


of the airways.
• Result: relief of bronchospasm and greater airflow
into and out of the lungs.
• Also causes CNS stimulation.
• Also causes cardiovascular stimulation: increased
force of contraction and increased HR, resulting in
increased cardiac output and increased blood flow to
the kidneys (diuretic effect).

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Bronchodilators: Xanthine Derivatives
Therapeutic Uses

• Dilation of airways in asthmas, chronic


bronchitis, and emphysema
• Mild to moderate cases of asthma
• Adjunct agent in the management of COPD
• Adjunct therapy for the relief of pulmonary
edema and paroxysmal nocturnal edema in
left-sided heart failure
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Bronchodilators: Xanthine Derivatives
Side Effects

• Nausea, vomiting, anorexia


• Gastroesophageal reflux during sleep
• Sinus tachycardia, extrasystole, palpitations,
ventricular dysrhythmias
• Transient increased urination

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Bronchodilators: Beta-Agonists

• Large group, sympathomimetics


• Used during acute phase of asthmatic
attacks
• Quickly reduce airway constriction and
restore normal airflow
• Stimulate beta2 adrenergic receptors
throughout the lungs

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Bronchodilators: Beta-Agonists
Three types
• Nonselective adrenergics
– Stimulate alpha1, beta1 (cardiac), and beta2 (respiratory)
receptors.
Example: epinephrine
• Nonselective beta-adrenergics
– Stimulate both beta1 and beta2 receptors.
Example: isoproterenol (Isuprel)
• Selective beta2 drugs
– Stimulate only beta2 receptors.
Example: albuterol

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Bronchodilators: Beta-Agonists
Mechanism of Action
• Begins at the specific receptor stimulated
• Ends with the dilation of the airways

Activation of beta2 receptors activate cAMP, which


relaxes smooth muscles of the airway and results
in bronchial dilation and increased airflow.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Bronchodilators: Beta-Agonists
Therapeutic Uses
• Relief of bronchospasm, bronchial asthma,
bronchitis, and other pulmonary disease.
• Useful in treatment of acute attacks as well
as prevention.
• Used in hypotension and shock.
• Used to produce uterine relaxation to prevent
premature labor.
• Hyperkalemia—stimulates potassium to shift into
the cell.
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Bronchodilators: Beta-Agonists
Side Effects
Alpha-Beta Beta1 and Beta2 Beta2
(epinephrine) (isoproterenol) (albuterol)

insomnia cardiac stimulation hypotension


restlessness tremor vascular
headache
anorexia anginal pain tremor
cardiac stimulation vascular headache tremor
vascular headache

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Respiratory Agents:
General Nursing Implications
• Encourage patients to take measures that
promote a generally good state of health in
order to prevent, relieve, or decrease
symptoms of COPD.
– Avoid exposure to conditions that precipitate
bronchospasms (allergens, smoking, stress, air pollutants)
– Adequate fluid intake
– Compliance with medical treatment
– Avoid excessive fatigue, heat, extremes in temperature,
caffeine

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Respiratory Agents:
General Nursing Implications
• Encourage patients to get prompt treatment
for flu or other illnesses, and to get
vaccinated against pneumonia or flu.
• Encourage patients to always check with
their physician before taking any other
medication, including OTC.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Respiratory Agents:
General Nursing Implications
• Perform a thorough assessment before
beginning therapy, including:
– Skin color
– Baseline vital signs
– Respirations (should be <12 or >24 breaths/min)
– Respiratory assessment, including PO2
– Sputum production
– Allergies
– History of respiratory problems
– Other medications
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
Respiratory Agents:
General Nursing Implications
• Teach patients to take bronchodilators
exactly as prescribed.
• Ensure that patients know how to use
inhalers, MDIs, and have the patients
demonstrate use of devices.
• Monitor for side effects.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Respiratory Agents:
Nursing Implications
• Monitor for therapeutic effects
– Decreased dyspnea
– Decreased wheezing, restlessness, and anxiety
– Improved respiratory patterns with return to
normal rate and quality
– Improved activity tolerance

• Decreased symptoms and increased


ease of breathing
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Bronchodilators: Nursing Implications
Xanthine Derivatives

• Contraindications: history of PUD or


GI disorders
• Cautious use: cardiac disease
• Timed-release preparations should not be
crushed or chewed (causes gastric irritation)

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Bronchodilators: Nursing Implications
Xanthine Derivatives

• Report to physician:
Palpitations Nausea Vomiting
Weakness Dizziness Chest pain
Convulsions

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Bronchodilators: Nursing Implications
Xanthine Derivatives

• Be aware of drug interactions with:


cimetidine, oral contraceptives, allopurinol
• Large amounts of caffeine can have
deleterious effects.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Bronchodilators: Nursing Implications
Beta-Agonist Derivatives

• Albuterol, if used too frequently, loses its


beta2-specific actions at larger doses.
• As a result, beta1 receptors are stimulated,
causing nausea, increased anxiety,
palpitations, tremors, and increased
heart rate.

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Bronchodilators: Nursing Implications
Beta-Agonist Derivatives

• Patients should take medications exactly


as prescribed, with no omissions or double
doses.
• Patients should report insomnia, jitteriness,
restlessness, palpitations, chest pain, or
any change in symptoms.

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Anticholinergics:
Mechanism of Action
• Acetylcholine (ACh) causes bronchial
constriction and narrowing of the airways.
• Anticholinergics bind to the ACh receptors,
preventing ACh from binding.
• Result: bronchoconstriction is prevented,
airways dilate.

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Anticholinergics

• Ipratropium bromide (Atrovent) is the only


anticholinergic used for respiratory disease.

• Slow and prolonged action

• Used to prevent bronchoconstriction

• NOT used for acute asthma exacerbations!

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Anticholinergics: Side Effects

Dry mouth or throat Gastrointestinal distress


Headache Coughing
Anxiety

No known drug interactions

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Antileukotrienes

• Also called leukotriene receptor antagonists


(LRTAs)
• New class of asthma medications
• Three subcategories of agents

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Antileukotrienes

Currently available agents:


• montelukast (Singulair)
• zafirlukast (Accolate)
• zileuton (Zyflo)

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Antileukotrienes:
Mechanism of Action
• Leukotrienes are substances released when
a trigger, such as cat hair or dust, starts a
series of chemical reactions in the body.
• Leukotrienes cause inflammation,
bronchoconstriction, and mucus production.
• Result: coughing, wheezing, shortness
of breath

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Antileukotrienes:
Mechanism of Action
• Antileukotriene agents prevent leukotrienes
from attaching to receptors on cells in the
lungs and in circulation.
• Inflammation in the lungs is blocked, and
asthma symptoms are relieved.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Antileukotrienes: Drug Effects

By blocking leukotrienes:
• Prevent smooth muscle contraction of the
bronchial airways
• Decrease mucus secretion
• Prevent vascular permeability
• Decrease neutrophil and leukocyte infiltration
to the lungs, preventing inflammation

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Antileukotrienes: Therapeutic Uses

• Prophylaxis and chronic treatment of asthma


in adults and children over age 12
• NOT meant for management of acute
asthmatic attacks
• Montelukast is approved for use in children
age 2 and older

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Antileukotrienes: Side Effects

zileuton zafirlukast
Headache Headache
Dyspepsia Nausea
Nausea Diarrhea
Dizziness Liver dysfunction
Insomnia
Liver dysfunction

montelukast has fewer side effects


Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
Antileukotrienes:
Nursing Implications
• Ensure that the drug is being used for
chronic management of asthma, not
acute asthma.
• Teach the patient the purpose of the therapy.
• Improvement should be seen in about
1 week.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Antileukotrienes:
Nursing Implications
• Check with physician before taking any
OTC or prescribed medications—many
drug interactions.
• Assess liver function before beginning
therapy.
• Medications should be taken every night on
a continuous schedule, even if symptoms
improve.

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Corticosteroids
• Anti-inflammatory
• Used for CHRONIC asthma
• Do not relieve symptoms of acute
asthmatic attacks
• Oral or inhaled forms
• Inhaled forms reduce systemic effects
• May take several weeks before full
effects are seen
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
Corticosteroids:
Mechanism of Action
• Stabilize membranes of cells that release
harmful bronchoconstricting substances.
• These cells are leukocytes, or white
blood cells.
• Also increase responsiveness of bronchial
smooth muscle to beta-adrenergic
stimulation.

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Inhaled Corticosteroids

• beclomethasone dipropionate
(Beclovent, Vanceril)
• triamcinolone acetonide
(Azmacort)
• dexamethasone sodium phosphate
(Decadron Phosphate Respihaler)
• flunisolide (AeroBid)

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Inhaled Corticosteroids:
Therapeutic Uses
• Treatment of bronchospastic disorders
that are not controlled by conventional
bronchodilators.
• NOT considered first-line agents for
management of acute asthmatic attacks
or status asthmaticus.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Inhaled Corticosteroids:
Side Effects
• Pharyngeal irritation
• Coughing
• Dry mouth
• Oral fungal infections
Systemic effects are rare because of the low
doses used for inhalation therapy.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Inhaled Corticosteroids:
Nursing Implications
• Contraindicated in patients with psychosis,
fungal infections, AIDS, TB.
• Cautious use in patients with diabetes,
glaucoma, osteoporosis, PUD, renal
disease, CHF, edema.
• Teach patients to gargle and rinse the mouth
with water afterward to prevent the
development of oral fungal infections.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Inhaled Corticosteroids:
Nursing Implications
• Abruptly discontinuing these medications
can lead to serious problems.
• If discontinuing, should be weaned for a
period of 1 to 2 weeks, and only if
recommended by physician.
• REPORT any weight gain of more than 5
pounds a week or the occurrence of chest
pain.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Mast Cell Stabilizers

• cromolyn (Nasalcrom, Intal)


• nedocromil (Tilade)

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Mast Cell Stabilizers

• Indirect-acting agents that prevent the


release of the various substances that
cause bronchospasm
• Stabilize the cell membranes of
inflammatory cells (mast cells, monocytes,
macrophages), thus preventing release of
harmful cellular contents
• No direct bronchodilator activity
• Used prophylactically

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Mast Cell Stabilizers:
Therapeutic Uses
• Adjuncts to the overall management
of COPD
• Used solely for prophylaxis, NOT for
acute asthma attacks
• Used to prevent exercise-induced
bronchospasm
• Used to prevent bronchospasm associated
with exposure to known precipitating factors,
such as cold, dry air or allergens
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
Mast Cell Stabilizers: Side Effects

Coughing Taste changes


Sore throat Dizziness
Rhinitis Headache
Bronchospasm

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Mast Cell Stabilizers:
Nursing Implications
• For prophylactic use only
• Contraindicated for acute exacerbations
• Not recommended for children under age 5
• Therapeutic effects may not be seen for up to
4 weeks
• Teach patients to gargle and rinse the mouth
with water afterward to minimize irritation to
the throat and oral mucosa
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

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